Discovery of <i>N</i>-(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays

Louis J. Lombardo, Francis Y. Lee, Ping Chen, +24

Journal of Medicinal Chemistry

Drug TargetPreclinical AssaysPharmacotherapyCompound 13Pharmaceutical Chemistry +17

2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of <i>N</i> -(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a Potent <i>pan</i> -Src Kinase Inhibitor

Jagabandhu Das, Ping Chen, Derek Norris, +18

Journal of Medicinal Chemistry

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56lck inhibitors

Jagabandhu Das, Robert V. Moquin, James C. Lin, +10

Bioorganic & Medicinal Chemistry Letters

Potent P56lck InhibitorsMedicinal ChemistryBiochemistryMedicineNatural Sciences +6

Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-<i>f</i>][1,2,4]triazine p38α Mitogen-Activated Protein Kinase Inhibitors

John Hynes, Alaric J. Dyckman, Shuqun Lin, +25

Journal of Medicinal Chemistry

5-Cyanopyrimidine Derivatives as a Novel Class of Potent, Selective, and Orally Active Inhibitors of p38α MAP Kinase

Chunjian Liu, Stephen T. Wrobleski, James C. Lin, +17

Journal of Medicinal Chemistry

5-Cyanopyrimidine DerivativesDrug TargetP38 InhibitorsCellular PharmacologyPharmacotherapy +17

Molecular design, synthesis, and structure–Activity relationships leading to the potent and selective p56lck inhibitor BMS-243117

Jagabandhu Das, James C. Lin, Robert V. Moquin, +11

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryBiochemistryMedicineDrug Discovery +12

Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-<i>N</i>-propylpyrrolo[1,2-<i>f</i>][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases

Chunjian Liu, James C. Lin, Stephen T. Wrobleski, +25

Journal of Medicinal Chemistry

P38α Enzymatic AssayPharmacotherapyInflammatory ArthritisInflammationMolecular Pharmacology +16

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck

John Wityak, Jagabandhu Das, Robert V. Moquin, +12

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryDrug TargetBiochemistryInitial SarNatural Sciences +9

The Discovery of Orally Active Triaminotriazine Aniline Amides as Inhibitors of p38 MAP Kinase

Katerina Leftheris, Gulzar Ahmed, Ran Chan, +35

Journal of Medicinal Chemistry

P38 Map KinaseTriaminotriazine AnilinePharmacotherapyChemical BiologyPharmaceutical Chemistry +17

Benzothiazole based inhibitors of p38α MAP kinase

Chunjian Liu, James C. Lin, Sidney Pitt, +13

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyBiochemistryMedicinePharmacological AgentPharmacotherapy +4